In-vitro and In-vivo Evaluation of Niosomal Gel Containing Aceclofenac for Sustained Drug Delivery

Abstract

Background: Niosomes are non-ionic stable vesicular system, which can accommodate both hydrophobic and hydrophilic drugs. The aim of the present study was to prepare and characterize niosomal gel formulations for sustained delivery of aceclofenac. Aceclofenac is the most widely used anti-inflammatory agent in the treatment of rheumatoid arthritis. It has narrow therapeutic index and short biological half-life. Methods: Aceclofenac loaded niosomes were prepared using reverse phase evaporation technique. The effects of concentration of non-ionic surfactant, cholesterol and concentration of drug on the encapsulation efficiency were studied. The formulations were characterized using different techniques, such as differential scanning calorimetry (DSC), fourier-transform infrared spectroscopy (FTIR), optical microscope and transmission electron microscope (TEM). Selected formulations of niosomes were incorporated into carbopol 934 (1%w/w), sodium alginate (7%w/w), sodium carboxy methyl cellulose (3% w/w), pluronic F127 (20%w/w) and HPMC (3% w/w) gels. The niosomal gel formulations were evaluated for in-vitro drug release and skin permeation. Optimum niosomal gel formulation was evaluated in-vivo using carrageenen-induced rat paw edema test and compared to gel containing the drug alone. Results: TEM analysis confirmed that niosomal samples were spherical in shape and have a definite internal aqueous space. Niosomes of span60 showed higher percent drug entrapment and larger particle size. In-vitro drug release and skin permeation of different gel preparations showed sustained release and enhanced permeation compared to gel formulations containing free drug. Among the niosomal gel formulations, HPMC gel showed the highest release rate of the drug. The in-vivo anti-inflammatory activity of the selected niosomal gel formulation was significantly higher and more sustained than the corresponding non-niosomal gel formulation containing free drug. Conclusion:These results suggest that the niosome-containing gels are promising formulations for sustained local delivery of aceclofenac.

<p>Characterization, optimization, and in vitro evaluation of Technetium-99m-labeled niosomes</p>

“…Liposomes in an aqueous system have been shown to have low physical and chemical stability due to problems such as hydrolysis of fatty acid esters and oxidative degradation of unsaturated fatty acids of the phospholipid component. [2][3][4][5][6][7][8] Alternatively, niosomes replace chemically unstable phospholipids with nonionic surfactants, which are also easier to handle and store and are more readily available at lower costs. [9][10][11][12] A majority of tumor-targeted nanocarriers rely on passive targeting that can be achieved by exploiting the pathophysiological characteristics of a solid tumor.…”

The Efficacy of Cholesterol-Based Carriers in Drug Delivery

“…Niosomes of Span 60:cholesterol of ratio 0.5:0.5 had the highest entrapment efficiency, as high as 95.6% when encapsulated with 15 mg of the drug. Increasing cholesterol content generally increased noisome size with the highest being 22.39 µm [ 110 ]. In vitro drug release studies showed that the release pattern of aceclofenac ranked as: HPMC > sodium alginate > sodium CMC > carbopol 934 > pluronic F-127 gels.…”

Pivotal role of Acitretin nanovesicular gel for effective treatment of psoriasis: ex vivo&ndash;in vivo evaluation study

“…65 Moreover, competition between higher amounts of CH and the drug for the packing spaces within the bilayers might prompt exclusion of the drug as amphiphiles assemble into the vesicles. 66,67 Particle size, PDI, and zeta potential Table 2 illustrates the particle size, PDI, and zeta potential of different Act-loaded niosomes. The PDI values of all the prepared niosomes were in the range of 0.1-0.5, therefore pointing to a narrow size distribution and good homogeneity.…”